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Other medications for smoking cessation

Bupropion (Zyban)

Candidates for bupropion

Bupropion can be offered to all patients who smoke (other than those with contraindications). Factors that make it a good first-line choice include:

  • current symptoms of depression or anxiety
  • history of intolerance of, or lack of success with, NRT
  • recent myocardial infarction or other coronary syndrome
  • patient concern about weight gain
  • patient preference.

Contraindications include:

  • history of seizures
  • current treatment for mental health symptoms with bupropion
  • history of severe adverse reactions to bupropion
  • current treatment with an MAO inhibitor.

Relative contraindications include:

  • current alcohol or benzodiazepine abuse or dependence
  • history of bipolar disorder
  • history of an eating disorder.

Prescribing bupropion

  • Discuss the risks and benefits of the medication with the patient.
  • Explain the very small increased risk of having a seizure while on bupropion.
  • Attempt to negotiate a quit date with the patient.
  • Start at 150 mg each morning for three to five days.
  • If tolerated, increase the dose to 150 mg twice daily after three to five days.
  • Explain that doses should be at least eight hours apart, ideally 150 mg before breakfast and 150 mg before dinner.
  • Consider switching to a long-acting bupropion (i.e., Wellbutrin XL 300 mg) daily after the dose is stabilized because once-per-day dosing is more convenient for patients, thus enhancing adherence, and Wellbutrin XL is often covered by health care plans.

Typical quit plan using bupropion

  • Start bupropion tomorrow morning.
  • Set quit date in 10 days.
  • Follow up with primary care provider in two weeks.

Combining bupropion with other smoking cessation medication

Bupropion has been shown to be effective when combined with NRT (Jorenby et al., 1999).

Varenicline (Champix)

How varenicline works

Varenicline is a partial nicotine agonist that is selective for the alpha4beta2 nicotinic acetylcholine receptor. It blocks the binding of exogenous nicotine to the receptor, with a subsequent reduction in the stimulation of the mesolimbic dopamine system in response to inhaling nicotine. Varenicline also provides a low level of stimulation in the absence of inhaled nicotine.

In short, varenicline provides a mild nicotine replacement effect while inhibiting the pleasurable effects of smoking.

Candidates for varenicline

Like most smoking cessation aids, varenicline is most successful in the context of a well-developed plan to quit smoking.

A recent multinational clinical trial (Ebbert et al., 2015) found that among cigarette smokers who were not willing or able to quit within the next month but were willing to reduce their smoking and make a quit attempt at three months, using varenicline compared to placebo for 24 weeks significantly increased smoking cessation rates, which held at one-year follow-up.

Varenicline is useful for patients who have been unsuccessful at quitting using NRT or bupropion. As these modalities have been available for several years, most patients interested in quitting smoking will already have tried these medications.

Varenicline is also useful for patients who:

  • have contraindications to the use of bupropion
  • do not tolerate bupropion or NRT
  • have an aversion to these medications due to their psychoactive effects.

Varenicline can be used as a first-line therapy in smoking cessation. Clinical trials have shown higher abstinence rates with varenicline than with either NRT or bupropion.

As there is no evidence linking the effectiveness of different medications with, for example, different patterns of smoking behaviour, the choice of medication should be influenced by patient preference.

Advising patients how to take varenicline

Tell patients the following:

  • Take varenicline after meals with a glass of water.
  • Varenicline takes seven to 10 days to start to work.
  • Do not use NRT products with varenicline because they increase the risk of nausea.
  • Stay on varenicline for at least 12 weeks.
  • If you succeed in quitting smoking, strongly consider using varenicline for another 12 weeks.
  • The most common side-effects are nausea, constipation, flatulence and increased dreams.
  • Side-effects tend to settle after two to three weeks.
  • If the side-effects are intolerable, try a lower dose before discontinuing the medication.

Practice recommendations for health care providers

The U.S. Food and Drug Administration ([FDA], 2015) recently updated the labeling for varenicline to include the following recommendations for health care providers:

  • Advise patients to reduce the amount of alcohol they consume while taking varenicline until they know whether the drug affects their tolerance for alcohol.
  • Weigh the potential risk of seizures against the potential benefits before prescribing varenicline in patients with a history of seizures or other factors that can lower the seizure threshold.
  • Advise patients to discontinue varenicline and seek medical attention immediately if they experience a seizure while on treatment.
  • Advise patients to immediately stop taking varenicline if they develop agitation, hostility, aggressive behaviour, depressed mood, or changes in behavior or thinking that are not typical for them, or if they develop suicidal ideation or behaviour.
  • Encourage patients to read the medication guide they receive with their varenicline prescription.
  • Report adverse events involving varenicline to the FDA MedWatch program.